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Peptide Testing Services

Peptides are a unique class of pharmaceutical compounds that have gained considerable interest due to their potential across a spectrum of diseases, including metabolic disorders, cardiovascular issues, cancer, and infectious diseases. Our comprehensive peptide testing services cover the entire scope of drug development, from discovery to IND application to NDA submission, allowing you to advance novel therapies further, faster.

Peptide Testing Services by WuXi AppTec Lab Testing Division

IND-Enabling Packages for Peptides

In Vitro Studies for Peptides

In Vivo Studies for Peptides

Why Peptides Need Specialized Development Support

Peptides are highly specific and biologically active—but their success depends on solving critical development challenges. At WuXi AppTec, our experienced teams and global network of peptide labs help you overcome these challenges with seamless, efficient testing solutions.

  • High molecular weight in comparison to traditional small molecules and polarity limit permeability
  • Rapid enzymatic degradation reduces stability
  • Complex bioanalytical properties challenge assay design
  • Risk of immunogenicity (anti-drug antibodies)
  • Specialized toxicology assessments required

Overcoming Peptide Development Challenges

Peptides present a number of challenges during preclinical development that can easily turn into costly delays and additional testing—especially if you don’t have an experienced guide. Here’s how we can help.

Stage: In Vitro

 

Peptide-Specific Challenge

  • Rapid enzymatic degradation
  • Poor permeability due to high polarity
  • High protein binding and non-specific adsorption

WuXi AppTec’s solution

  • Advanced stability testing in plasma, liver/kidney S9 fractions, hepatocytes, and simulated gastric/intestinal fluids
  • Permeability assessment using Caco-2, MDCK, and EPSA measurements for passive and endocytotic uptake
  • Radiolabeling (e.g., 14C) to enable definitive metabolism and soft-spot studies
  • Custom assay development to characterize metabolic pathways and degradation profiles

Stage: In Vivo

 

Peptide-Specific Challenge

  • Low systemic exposure after administration
  • Complex tissue distribution, especially for oral and injectable routes
  • Barriers to achieving therapeutic concentrations at target sites

WuXi AppTec’s solution

  • Tailored IV, SC, and oral PK study design in relevant species
  • Radiolabeling strategies for tissue distribution, excretion, and QWBA studies
  • Formulation support for bioavailability enhancement (e.g., permeability enhancers, cyclic peptide design)

Stage: Bioanalysis

 

Peptide-Specific Challenge

  • High structural diversity impacting assay sensitivity and specificity
  • Non-specific binding in plasma due to hydrophobic modifications or formulation excipients
  • Matrix effects complicating quantification
  • Need for robust ADA (anti-drug antibody) detection and immunogenicity monitoring

WuXi AppTec’s solution

  • Full LC-MS/MS and LBA platforms optimized for peptides, including hybrid LBALCMS (immunocapture + MS readout) for sensitivity & selectivity
  • Advanced sample preparation to minimize non-specific binding (e.g., NSB blockers, low-binding tubes)
  • Method development to overcome matrix effects, ensuring assay robustness and reproducibility

Stage: Early Toxicology

 

Peptide-Specific Challenge

  • Selecting relevant species given differences in peptide metabolism and immunogenicity
  • Assessing local toxicity for SC/IV/oral administration
  • Evaluating dose ranges in exploratory studies

WuXi AppTec’s solution

  • Species selection guided by PK and immunogenicity profiles to ensure relevance
  • Early safety pharmacology studies covering CNS, cardiovascular, and respiratory systems
  • Immunogenicity risk assessments and ADA monitoring in non-GLP settings

Stage: GLP Toxicology

 

Peptide-Specific Challenge

  • Meeting regulatory expectations for repeat-dose toxicity and immunogenicity assessments
  • Managing potential off-target effects and local irritation
  • Addressing genotoxicity risks with non-natural amino acids

WuXi AppTec’s solution

  • GLP-compliant repeat-dose studies in rodents and non-rodents with immunogenicity monitoring
  • Robust species selection strategy in line with ICH guidelines (M3, S6)
  • Genetic toxicology studies tailored to peptide modifications and non-natural amino acids
  • Comprehensive reproductive, carcinogenicity, and local toxicity studies as required for IND submission

Stage: IND Submission

 

Peptide-Specific Challenge

  • Ensuring consistency and integration across DMPK, bioanalysis, and toxicology data
  • Preparing clear, complete packages for regulatory submission
  • Addressing evolving regulatory expectations for peptide therapeutics

WuXi AppTec’s solution

  • Integrated project teams coordinating DMPK, bioanalysis, and toxicology
  • Regulatory strategy consulting to address immunogenicity, ADA assessments, and safety study design
  • Flexible, scalable capabilities to support submissions worldwide

Comprehensive Preclinical
Testing for Peptides

Peptides are composed of a series of well-ordered amino acids with molecular weights between 500 and 5,000 Da – a unique structure that requires specialized preclinical testing techniques. With capabilities in DMPK/ADME, bioanalysis, safety assessment, pharmacology, and CMC, WuXi AppTec can support every aspect of peptide development – all conveniently under one roof.

Bioanalysis

We develop and validate robust analytical methods tailored to the unique characteristics of peptides, with high specificity and sensitivity.

DMPK

Access a global network of testing facilities for peptide DMPK research, focusing on peptide stability, permeation, delivery carrier, and tissue distribution studies.

Toxicology

Our peptide-tailored safety assessment services include immunogenicity, off-target effects, metabolic stability, administration routes, dose-dependency, and more.

New Insights for New Modalities

WEBINAR

Peptide Therapeutics: Navigating Development with DMPK & Toxicology

BROCHURE

Preclinical Drug Development Testing for Peptide

BLOG

Bioanalysis of GLP-1 Antagonist Drugs by Multiple Analytical Platforms

BLOG

Bioanalytical Strategies for Peptide-Drug Conjugates (PDCs): Optimized Approaches for the Pharmaceutical Industry

Frequently Asked Questions

What are peptides?

Therapeutic peptides are a unique class of pharmaceutical compounds composed of a series of well-ordered amino acids, usually with molecular weights of 500 – 5,000 Da. They act as agonists or antagonists of particular receptors, enzymes, or proteins, thereby modulating physiological processes. 

What are the biggest therapeutic opportunities related to peptides?

Peptide drugs have gained considerable interest due to their potential across a spectrum of diseases, including metabolic disorders, cardiovascular issues, cancer, and infectious diseases. The recent blockbuster drug glucagon-like peptide-1 (GLP-1) hormone stands as a great example of the efficacy and promise offered by peptide therapeutics in clinical practice.

Why is preclinical testing important for peptides?

Preclinical testing is crucial for peptides to evaluate their safety, efficacy, and pharmacokinetics before they enter clinical trials. It helps identify any potential toxic effects, optimal dosing regimens, and therapeutic potential, ensuring that only promising candidates proceed to human trials.

Why is an experienced peptide testing partner important for your program’s success?

In addition to ensuring that your therapeutic peptides undergo rigorous, unbiased analysis, the biggest reason to work with an experienced testing partner is to identify potential issues as early as possible. Doing so will help accelerate your development timeline and significantly increase your program’s likelihood of success. Beyond this, utilizing 3rd-party tested peptides will also help you maintain regulatory compliance, ensure data integrity, and provide confidence in your results.

How is preclinical testing for peptides different from other types of molecules?

Preclinical DMPK research on peptides mainly focuses on stability, permeation, delivery carrier, and tissue distribution studies. Bioanalytical method development focuses on detecting and quantifying the peptide in biological samples with high specificity and sensitivity.

What are some challenges of peptide development and testing?

One of the unique bioanalysis challenges for peptide development during preclinical studies is the need for highly sensitive and specific analytical methods to detect and quantify peptides in biological matrices. Peptides are larger and more structurally complex molecules compared to small molecules. 

Other challenges specific to DMPK research include: 

  • Peptide molecules are physiologically active. Therefore, the dosage is small, and the drug concentration in vivo is rather low. Additionally, there are a large number of endogenous interfering substances in organisms. Both the specificity and sensitivity of the analysis method must be high.
  • Multiple charged ions are likely to be generated in the mass spectrometry ion source by peptide molecules. Also, ions of different valence states are dispersed to a certain extent, making it difficult to determine the optimal ion pair. 
  • Peptide molecules also have some other common problems such as non-specific adsorption, low stability, and a high protein binding ratio, posing serious challenges for sample processing and detection. 
  • Peptides cannot easily cross various bio-membrane barriers in the body as they are highly polarized and poorly permeable. Thus, the oral bioavailability of peptides needs to be improved. 
  • Peptides have poor metabolic stability, wide metabolic pathways, and short half-life periods.

What types of preclinical studies are essential for peptides?

Preclinical research on peptides mainly focuses on stability, permeation, delivery carrier, and tissue distribution studies. 

  • Early screening stage: Mainly investigating the in vitro properties of peptide molecules (including plasma stability, metabolic stability, permeation, and protein binding) and guiding molecular structure optimization. The interactions and enzyme phenotyping of peptides with low molecular weight are evaluated as well. 
  • PCC stage: This stage focuses on the metabolic differences of species and the in vivo PK study of peptides. It aims to select the appropriate species for relevant research by considering both pharmacodynamics and toxicology. The study of various delivery carriers makes it possible to achieve the desired in vivo exposure characteristics.
  • IND stage: In this stage, single dose escalation and repeated administration PK in animals will be studied. The excretion pathway (mass balance), tissue distribution, and in vivo metabolites identification also need be evaluated.

What safety assessments are critical in the preclinical testing of peptides?

Immunogenicity tests are particularly important for peptides due to the potential for peptides to elicit immune responses. Acute and chronic toxicity studies are conducted to determine the toxic effects over different exposure periods. Genotoxicity studies evaluate any risk of genetic damage, and safety pharmacology studies monitor vital functions such as cardiovascular, respiratory, and central nervous systems.

What considerations are important for DMPK studies on peptides?

For Drug Metabolism and Pharmacokinetics (DMPK) studies on peptides, it is important to consider the peptide’s stability, bioavailability, and routes of administration. The potential for enzymatic degradation, the impact of formulation on absorption, and the peptide’s distribution and elimination pathways are also critical factors.

What regulatory guidelines must be followed for preclinical testing of peptides?

Preclinical testing of peptides must adhere to regulatory guidelines such as those from the FDA, EMA, and ICH, which include Good Laboratory Practice (GLP) standards. Specific guidelines for biologics, including peptides, cover aspects such as immunogenicity (ICH S6(R1)), toxicology studies (ICH M3(R2)), and the evaluation of safety pharmacology (ICH S7A).

What are the potential pharmacological concerns of peptides?

Pharmacological concerns specific to peptides include their rapid degradation by proteases in the body, leading to poor bioavailability and short half-lives. Peptides can also be immunogenic, potentially triggering unwanted immune responses. Their specificity to target receptors may cause off-target effects, and they often require advanced delivery systems to achieve therapeutic levels.

What efficacy tests are conducted for peptides in preclinical studies?

Efficacy tests for peptides involve in vitro assays to assess their interaction with target receptors or enzymes and to measure biological activity. In vivo studies use animal models of the target disease to evaluate therapeutic outcomes, such as reduction in disease biomarkers, improvement in clinical symptoms, and overall survival rates, providing a comprehensive assessment of the peptide’s therapeutic potential.

What analytical methods are used in peptide preclinical testing?

Peptides require the development and validation of robust analytical methods tailored to their unique characteristics. This may involve optimizing sample preparation techniques, selecting appropriate analytical platforms such as liquid chromatography-mass spectrometry (LC-MS) or enzyme-linked immunosorbent assay (ELISA), and implementing stringent quality control measures to ensure the accuracy and reliability of peptide quantification in preclinical studies.

Let’s Talk About Your Peptide Program

Have questions? Need specific assays? Talk to an expert today about your peptide needs.